کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5822386 | 1117940 | 2013 | 42 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Development of a fluorescence-based HIV-1 integrase DNA binding assay for identification of novel HIV-1 integrase inhibitors
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کلمات کلیدی
PBSIntegrase strand transfer inhibitorsINSTIsRFULTRHTSBSA - BSADMSO - DMSObovine serum albumin - آلبومین سرم گاوIntegrase - انتگرالReverse transcriptase - ترانس کریپتاز معکوس یا وارونویسFluorescent assay - تست فلورسنتLong terminal repeat - تکرار طولانی مدتDimethyl sulfoxide - دیمتیل سولفواکسیدhigh-throughput screening - غربالگری بالاPhosphate buffered saline - فسفات بافر شورHIV-1 integrase inhibitors - مهار کننده های انتگرال HIV-1Relative Fluorescence Units - واحد فلورسانس نسبیhuman immunodeficiency virus - ویروس نقص ایمنی انسانیHIV - ویروس نقص ایمنی انسانی
موضوعات مرتبط
علوم زیستی و بیوفناوری
ایمنی شناسی و میکروب شناسی
ویروس شناسی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
Human immunodeficiency virus integrase (HIV-1 IN) inhibitors that are currently approved or are in advanced clinical trials specifically target the strand transfer step of integration. However, considerable cross-resistance exists among some members of this class of IN inhibitors. Intriguingly, though, HIV-1 IN possesses multiple sites, distinct from those involved in the strand transfer step, that could be targeted to develop new HIV-1 IN inhibitors. We have developed a fluorescent HIV-1 IN DNA binding assay that can identify small molecules termed IN binding inhibitors (INBIs) that inhibit IN binding to viral DNA. This assay has been optimized with respect to concentrations of each protein, long terminal repeat (LTR) DNA substrate, salt, and time, and has been used successfully to measure the HIV-1 IN DNA binding activity of a well-characterized INBI termed FZ41. In addition, we have used the assay to screen a small library of natural products, resulting in the identification of nigranoic acid as a new INBI. The proposed fluorescence assay is easy and inexpensive, and provides a high-throughput detection method for determination of HIV-1 IN DNA binding activity, monitoring of enzyme kinetics, and high-throughput screening for the identification of new INBIs.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Antiviral Research - Volume 98, Issue 3, June 2013, Pages 441-448
Journal: Antiviral Research - Volume 98, Issue 3, June 2013, Pages 441-448
نویسندگان
Ying-Shan Han, Wei-Lie Xiao, Peter K. Quashie, Thibault Mesplède, Hongtao Xu, Eric Deprez, Olivier Delelis, Jian-Xin Pu, Han-Dong Sun, Mark A. Wainberg,